CN1562043A - Epristeride dripping pills and its preparing method - Google Patents
Epristeride dripping pills and its preparing method Download PDFInfo
- Publication number
- CN1562043A CN1562043A CN 200410030368 CN200410030368A CN1562043A CN 1562043 A CN1562043 A CN 1562043A CN 200410030368 CN200410030368 CN 200410030368 CN 200410030368 A CN200410030368 A CN 200410030368A CN 1562043 A CN1562043 A CN 1562043A
- Authority
- CN
- China
- Prior art keywords
- epristeride
- coolant
- time
- dissolution
- polyethylene glycol
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
- 239000006187 pill Substances 0.000 title claims abstract description 17
- VAPSMQAHNAZRKC-PQWRYPMOSA-N Epristeride Chemical compound C1C=C2C=C(C(O)=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H](C(=O)NC(C)(C)C)[C@@]1(C)CC2 VAPSMQAHNAZRKC-PQWRYPMOSA-N 0.000 title claims description 28
- 229950009537 epristeride Drugs 0.000 title claims description 28
- 238000000034 method Methods 0.000 title description 9
- 238000002360 preparation method Methods 0.000 claims description 12
- 239000002826 coolant Substances 0.000 claims description 11
- VBICKXHEKHSIBG-UHFFFAOYSA-N 1-monostearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(O)CO VBICKXHEKHSIBG-UHFFFAOYSA-N 0.000 claims description 10
- 238000001035 drying Methods 0.000 claims description 8
- 239000000843 powder Substances 0.000 claims description 8
- 229940093429 polyethylene glycol 6000 Drugs 0.000 claims description 7
- RVGRUAULSDPKGF-UHFFFAOYSA-N Poloxamer Chemical compound C1CO1.CC1CO1 RVGRUAULSDPKGF-UHFFFAOYSA-N 0.000 claims description 5
- 229940008099 dimethicone Drugs 0.000 claims description 5
- 235000013870 dimethyl polysiloxane Nutrition 0.000 claims description 5
- 239000004205 dimethyl polysiloxane Substances 0.000 claims description 5
- 238000002156 mixing Methods 0.000 claims description 5
- TZBAVQKIEKDGFH-UHFFFAOYSA-N n-[2-(diethylamino)ethyl]-1-benzothiophene-2-carboxamide;hydrochloride Chemical compound [Cl-].C1=CC=C2SC(C(=O)NCC[NH+](CC)CC)=CC2=C1 TZBAVQKIEKDGFH-UHFFFAOYSA-N 0.000 claims description 5
- 229960000502 poloxamer Drugs 0.000 claims description 5
- 229920001983 poloxamer Polymers 0.000 claims description 5
- 229920000435 poly(dimethylsiloxane) Polymers 0.000 claims description 5
- 239000000758 substrate Substances 0.000 claims description 5
- 239000011159 matrix material Substances 0.000 claims description 4
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 3
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims 2
- IQXJCCZJOIKIAD-UHFFFAOYSA-N 1-(2-methoxyethoxy)hexadecane Chemical compound CCCCCCCCCCCCCCCCOCCOC IQXJCCZJOIKIAD-UHFFFAOYSA-N 0.000 claims 1
- 239000001828 Gelatine Substances 0.000 claims 1
- 241000238631 Hexapoda Species 0.000 claims 1
- 235000021355 Stearic acid Nutrition 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- 230000001476 alcoholic effect Effects 0.000 claims 1
- 229950009789 cetomacrogol 1000 Drugs 0.000 claims 1
- 229920000159 gelatin Polymers 0.000 claims 1
- 235000019322 gelatine Nutrition 0.000 claims 1
- YQEMORVAKMFKLG-UHFFFAOYSA-N glycerine monostearate Natural products CCCCCCCCCCCCCCCCCC(=O)OC(CO)CO YQEMORVAKMFKLG-UHFFFAOYSA-N 0.000 claims 1
- 235000011187 glycerol Nutrition 0.000 claims 1
- 229960005150 glycerol Drugs 0.000 claims 1
- SVUQHVRAGMNPLW-UHFFFAOYSA-N glycerol monostearate Natural products CCCCCCCCCCCCCCCCC(=O)OCC(O)CO SVUQHVRAGMNPLW-UHFFFAOYSA-N 0.000 claims 1
- 229940057995 liquid paraffin Drugs 0.000 claims 1
- -1 liquid paraffin Substances 0.000 claims 1
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 claims 1
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 claims 1
- 229940093430 polyethylene glycol 1500 Drugs 0.000 claims 1
- RYYKJJJTJZKILX-UHFFFAOYSA-M sodium octadecanoate Chemical compound [Na+].CCCCCCCCCCCCCCCCCC([O-])=O RYYKJJJTJZKILX-UHFFFAOYSA-M 0.000 claims 1
- 229940080350 sodium stearate Drugs 0.000 claims 1
- 239000008117 stearic acid Substances 0.000 claims 1
- 235000015112 vegetable and seed oil Nutrition 0.000 claims 1
- 239000008158 vegetable oil Substances 0.000 claims 1
- 239000001993 wax Substances 0.000 claims 1
- 238000010298 pulverizing process Methods 0.000 abstract 1
- 238000004090 dissolution Methods 0.000 description 26
- 238000001514 detection method Methods 0.000 description 12
- 229940075507 glyceryl monostearate Drugs 0.000 description 4
- 239000001788 mono and diglycerides of fatty acids Substances 0.000 description 4
- 238000003756 stirring Methods 0.000 description 4
- 206010004446 Benign prostatic hyperplasia Diseases 0.000 description 3
- 239000003814 drug Substances 0.000 description 3
- 238000005516 engineering process Methods 0.000 description 3
- NVKAWKQGWWIWPM-ABEVXSGRSA-N 17-β-hydroxy-5-α-Androstan-3-one Chemical compound C1C(=O)CC[C@]2(C)[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CC[C@H]21 NVKAWKQGWWIWPM-ABEVXSGRSA-N 0.000 description 2
- 208000019505 Deglutition disease Diseases 0.000 description 2
- MUMGGOZAMZWBJJ-DYKIIFRCSA-N Testostosterone Chemical compound O=C1CC[C@]2(C)[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CCC2=C1 MUMGGOZAMZWBJJ-DYKIIFRCSA-N 0.000 description 2
- 229960003473 androstanolone Drugs 0.000 description 2
- 210000004369 blood Anatomy 0.000 description 2
- 239000008280 blood Substances 0.000 description 2
- 238000004891 communication Methods 0.000 description 2
- 229940079593 drug Drugs 0.000 description 2
- 238000009472 formulation Methods 0.000 description 2
- 210000001035 gastrointestinal tract Anatomy 0.000 description 2
- 238000004519 manufacturing process Methods 0.000 description 2
- 239000000203 mixture Substances 0.000 description 2
- 210000002307 prostate Anatomy 0.000 description 2
- 230000001225 therapeutic effect Effects 0.000 description 2
- 206010003694 Atrophy Diseases 0.000 description 1
- 208000004403 Prostatic Hyperplasia Diseases 0.000 description 1
- 238000010521 absorption reaction Methods 0.000 description 1
- 230000037444 atrophy Effects 0.000 description 1
- 210000001124 body fluid Anatomy 0.000 description 1
- 239000010839 body fluid Substances 0.000 description 1
- 230000002950 deficient Effects 0.000 description 1
- 238000009826 distribution Methods 0.000 description 1
- 230000003203 everyday effect Effects 0.000 description 1
- 230000029142 excretion Effects 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
- 230000010534 mechanism of action Effects 0.000 description 1
- 239000002547 new drug Substances 0.000 description 1
- 230000036963 noncompetitive effect Effects 0.000 description 1
- 239000000825 pharmaceutical preparation Substances 0.000 description 1
- 229940127557 pharmaceutical product Drugs 0.000 description 1
- 102000004169 proteins and genes Human genes 0.000 description 1
- 108090000623 proteins and genes Proteins 0.000 description 1
- 210000002966 serum Anatomy 0.000 description 1
- 150000003431 steroids Chemical class 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 229960003604 testosterone Drugs 0.000 description 1
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- Medicinal Preparation (AREA)
Abstract
A dripping pill of Aipuliete is prepared through superfine pulverizing and the conventional steps for preparing dripping pills.
Description
Technical field
The present invention relates to a kind of pharmaceutical product and preparation method thereof, specifically epristeride drop pill and preparation method thereof.
Background technology
Epristeride is noncompetitive steroid II type 5 inhibitor optionally, be used for the treatment of benign prostate hyperplasia, its mechanism of action is to be converted into the content that dihydrotestosterone reduces dihydrotestosterone in the body of prostate by suppressing testosterone, causes outgrowth body of prostate atrophy.
The pharmacokinetics of epristeride is two chamber models, and it absorbs rapidly at digestive tract, just can measure medicine in 0.25 hour after the administration to be present in the serum.3～4 hours blood drug level peakings are eliminated phase half-life (t
1/2β) be 7.5 hours, successive administration (5mg/ time, every day 2 times) the 6th day, blood drug level can reach stable state.Mainly drain, seldom through renal excretion through gastrointestinal tract.Average protein binding rate is up to 97%.Apparent volume of distribution approximates 0.5L/kg, and is suitable substantially with the body fluid volume of human body.List marketing at present tablet only arranged, the clinical benign prostate hyperplasia that is used for the treatment of improves the relevant symptom because of benign prostatic hyperplasia.
Epristeride sheet disintegration time is long, and dissolution and dissolution rate are low, absorption difference, and bioavailability is low, and the supplementary product consumption ratio is big, and old people, bed patient and dysphagia patients are taken inconvenience, and compliance is poor, has influenced the performance of epristeride therapeutical effect.
The present invention makes the epristeride drop pill by using ultramicro communication technique and dropping pill formulation Technology exactly, thereby overcomes the above defective of epristeride sheet, and the therapeutical effect of epristeride is given full play to.
Summary of the invention
The epristeride drop pill of making by using ultramicro communication technique and dropping pill formulation Technology not only have disintegrate molten loose fast, dissolution and dissolution rate improve, steady quality, the pill volume is little, both can swallow also can buccal, easy to carry and use, onset is rapid, compliance is good, be particularly suitable for the characteristics that old people, bed patient and dysphagia patients are taken, but also have working condition and production equipment is simple, production cost is low, compare the advantage that supplementary product consumption reduces with tablet, demonstrated fully the new drug research exploitation spirit that people-oriented.
For achieving the above object, the present invention by the following technical solutions: the epristeride fine powder of 1 weight portion through micronizing is added in 1～10 weight portion molten matrix, abundant mixing, dropping preparation method is condensed into ball in coolant, remove coolant, drying, promptly.
Three, example 1 sample detection result
1. the molten diffusing time: 2 minutes
2. dissolution rate:
Time (minute) 10 20 30 40
Dissolution (%) 53.4 82.6 98.7 97.2
Four, example 2 sample detection results
1. the molten diffusing time: 2 minutes
2. dissolution rate:
Time (minute) 10 20 30 40
Dissolution (%) 50.3 84.5 91.0 98.4
Five, example 3 sample detection results
1. the molten diffusing time: 3 minutes
2. dissolution rate:
Time (minute) 10 20 30 40
Dissolution (%) 48.6 82.7 95.4 96.2
Six, example 4 sample detection results
1. the molten diffusing time: 5 minutes
2. dissolution rate:
Time (minute) 10 20 30 40
Dissolution (%) 44.3 79.6 89.2 97.1
Seven, example 5 sample detection results
1. the molten diffusing time: 8 minutes
2. dissolution rate:
Time (minute) 10 20 30 40
Dissolution (%) 40.3 84.5 92.6 99.5
Eight, example 6 sample detection results
Three, example 1 sample detection result
1. the molten diffusing time: 2 minutes
2. dissolution rate:
Time (minute) 10 20 30 40
Dissolution (%) 53.4 82.6 98.7 97.2
Four, example 2 sample detection results
1. the molten diffusing time: 2 minutes
2. dissolution rate:
Time (minute) 10 20 30 40
Dissolution (%) 50.3 84.5 91.0 98.4
Five, example 3 sample detection results
1. the molten diffusing time: 3 minutes
2. dissolution rate:
Time (minute) 10 20 30 40
Dissolution (%) 48.6 82.7 95.4 96.2
Six, example 4 sample detection results
1. the molten diffusing time: 5 minutes
2. dissolution rate:
Time (minute) 10 20 30 40
Dissolution (%) 44.3 79.6 89.2 97.1
Seven, example 5 sample detection results
1. the molten diffusing time: 8 minutes
2. dissolution rate:
Time (minute) 10 20 30 40
Dissolution (%) 40.3 84.5 92.6 99.5
Eight, example 6 sample detection results
1. the molten diffusing time: 12 minutes
2. dissolution rate
Time (minute) 10 20 30 40
Dissolution (%) 51.7 82.3 94.5 95.2
The specific embodiment
One, example 1
Prescription:
Epristeride 5g
Polyethylene glycol 6000 15g
Make 1000
Method for making: the epristeride fine powder that the micronizing of learning from else's experience is crossed 200 mesh sieves is added in the fused polyethylene glycol 6000 substrate, stirs evenly, and with the dimethicone coolant, the dropping preparation method pill, drying, promptly.
Two, example 2
Prescription:
Epristeride 5g
Macrogol 4000 15g
Make 1000
Method for making: the epristeride fine powder that the micronizing of learning from else's experience is crossed 200 mesh sieves is added in the fused Macrogol 4000 substrate, stirs evenly, and with the dimethicone coolant, the dropping preparation method pill, drying, promptly.
Three, example 3
Prescription:
Epristeride 5g
Polyethylene glycol 6000 5g
Macrogol 4000 10g
Make 1000
Method for making: the epristeride fine powder that the micronizing of learning from else's experience is crossed 200 mesh sieves is added in fused Macrogol 4000 and the polyethylene glycol 6000 mixed-matrix, stirs evenly, and with the dimethicone coolant, the dropping preparation method pill, drying, promptly.
Four, example 4
Prescription:
Epristeride 5g
Glyceryl monostearate 15g
Make 1000
Method for making: the epristeride fine powder that the micronizing of learning from else's experience is crossed 200 mesh sieves is added in the fused glyceryl monostearate substrate, and mixing is a coolant with the frozen water, the dropping preparation method pill, and drying, promptly.
Five, example 5
Prescription:
Epristeride 5g
Polyethylene glycol 6000 10g
Poloxamer 5g
Make 1000
Method for making: the epristeride fine powder that the micronizing of learning from else's experience is crossed 200 mesh sieves is added in fused polyethylene glycol 6000 and the poloxamer mixed-matrix, stirs evenly, and with the dimethicone coolant, the dropping preparation method pill, drying, promptly.
Six, example 6
Prescription:
Epristeride 5g
Glyceryl monostearate 15g
Poloxamer 1g
Make 1000
Method for making: get the mixing fine powders that epristeride and poloxamer cross 200 mesh sieves through micronizing and be added in the fused glyceryl monostearate substrate, mixing is a coolant with the frozen water, the dropping preparation method pill, and drying, promptly.
Claims (4)
1. epristeride drop pill and preparation method thereof is characterized in that: the epristeride fine powder of 1 weight portion through micronizing is added in 1～10 weight portion molten matrix, and abundant mixing, dropping preparation method is condensed into ball in coolant, remove coolant, drying, promptly.
2. the molecular formula of the described epristeride Epristeride of claim 1 is C
25H
37NO
3, molecular weight is 399.57, structural formula is
3. the described substrate of claim 1 includes but not limited to polyethylene glycol 6000, Macrogol 4000, polyethylene glycol 1500, cetomacrogol 1000, sodium stearate, glycerin gelatine, poloxamer, stearic acid, glycerol monostearate acid, insect wax etc.
4. the described coolant of claim 1 includes but not limited to dimethicone, liquid paraffin, vegetable oil, water, alcoholic solution etc.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200410030368 CN1562043A (en) | 2004-03-29 | 2004-03-29 | Epristeride dripping pills and its preparing method |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200410030368 CN1562043A (en) | 2004-03-29 | 2004-03-29 | Epristeride dripping pills and its preparing method |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1562043A true CN1562043A (en) | 2005-01-12 |
Family
ID=34481095
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 200410030368 Pending CN1562043A (en) | 2004-03-29 | 2004-03-29 | Epristeride dripping pills and its preparing method |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1562043A (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100421666C (en) * | 2006-07-27 | 2008-10-01 | 江苏联环药业股份有限公司 | Epristeride slow release preparation |
| CN102038658A (en) * | 2009-10-20 | 2011-05-04 | 江苏联环药业股份有限公司 | Epristeride tablets with high dissolution rate and preparation method thereof |
-
2004
- 2004-03-29 CN CN 200410030368 patent/CN1562043A/en active Pending
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100421666C (en) * | 2006-07-27 | 2008-10-01 | 江苏联环药业股份有限公司 | Epristeride slow release preparation |
| CN102038658A (en) * | 2009-10-20 | 2011-05-04 | 江苏联环药业股份有限公司 | Epristeride tablets with high dissolution rate and preparation method thereof |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
| WD01 | Invention patent application deemed withdrawn after publication |